Studies designed to elucidate the mechanism-of-action of the antitumor antibiotic neocarzinostatin are proposed. A convergent and expeditious plan for the laboratory synthesis of the neocarzinostatin chromophore is presented which features methodology of general validity for structural congeners. The proposed studies will conclusively establish the stereochemical designation of the antibiotic and promise to be of value for the preparation of related new DNA-cleaving molecules and drug substances.